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Merck
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Key Documents

361571

Sigma-Aldrich

CHIR99021

≥95% (HPLC), liquid, GSK-3 inhibitor, Calbiochem

别名:

InSolution GSK-3抑制剂XVI,CHIR99021, 6-(2-(4-(2,4-二氯苯基)-5-(4-甲基-1H-咪唑-2-基)-嘧啶-2-基氨基)乙基-氨基)-烟酰胺腈

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About This Item

经验公式(希尔记法):
C22H18Cl2N8
分子量:
465.34
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.28

product name

GSK-3抑制剂XVI,CHIR99021, InSolution, ≥95%, 25 mM

品質等級

化驗

≥95% (HPLC)

形狀

liquid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light

運輸包裝

ambient

儲存溫度

−70°C

InChI

1S/C22H18Cl2N8/c1-13-10-29-21(31-13)17-12-30-22(32-20(17)16-4-3-15(23)8-18(16)24)27-7-6-26-19-5-2-14(9-25)11-28-19/h2-5,8,10-12H,6-7H2,1H3,(H,26,28)(H,29,31)(H,27,30,32)

InChI 密鑰

AQGNHMOJWBZFQQ-UHFFFAOYSA-N

一般說明

一种细胞可渗透的氨基嘧啶化合物,可作为有效、ATP竞争性和高度选择性的GSK-3抑制剂(对于GSK-3α和GSK-3β,IC50分别为10和6.7 nM)。对46种其他酶几乎没有活性(对于20种激酶,IC50 >8.8 µM,对于23种非激酶,Ki ≥5 µM),并且仅与22种药理学相关受体(Kd ~4 µM)弱结合。该化合物可口服获得,并显示可有效改善体内鼠和大鼠2型糖尿病模型中的葡萄糖代谢。另提供该化合物的固体形式(目录号361559)。

生化/生理作用

主要靶标
GSK-3 α 和 β
可逆性:是
细胞可渗透性:是
靶标IC50:10和6.7 nM,针对GSK-3&alpha

包裝

用惰性气体包装

警告

毒性:刺激性(B)

外觀

GSK-3抑制剂XVI,CHIR99021(目录号361559)在DMSO中的25 mM(5 mg/430 µL)溶液。

其他說明

Mussmann, R., et al. 2007.J. Biol. Chem.282, 12030.
Ring, D.B., et al. 2003.Diabetes52, 588.
Bennett, C.N., et al. 2002.J. Biol. Chem.277, 30998.
Cline, G.W., et al. 2002.
Diabetes51, 2903.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

儲存類別代碼

10 - Combustible liquids

水污染物質分類(WGK)

WGK 2

閃點(°F)

188.6 °F - closed cup - (refers to pure substance)

閃點(°C)

87 °C - closed cup - (refers to pure substance)


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